• Journal of Ginseng Research
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• v.43 no.2
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• pp.319-325
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• 2019

Background: Ginsenoside Rf is a ginseng saponin found only in Panax ginseng that affects lipid metabolism. It also has neuroprotective and antiinflammatory properties. We previously showed that Korean Red Ginseng (KRG) inhibited the expression of cyclooxygenase-2 (COX-2) by hypoxia via peroxisome proliferator-activated receptor gamma ($PPAR{\gamma}$). The aim of the current study was to evaluate the possibility of ginsenoside Rf as an active ingredient of KRG in the inhibition of hypoxia-induced COX-2 via $PPAR{\gamma}$. Methods: The effects of ginsenoside Rf on the upregulation of COX-2 by hypoxia and its antimigration effects were evaluated in A549 cells. Docking of ginsenoside Rf was performed with the $PPAR{\gamma}$ structure using Surflex-Dock in Sybyl-X 2.1.1. Results: $PPAR{\gamma}$ protein levels and peroxisome proliferator response element promoter activities were promoted by ginsenoside Rf. Inhibition of COX-2 expression by ginsenoside Rf was blocked by the $PPAR{\gamma}-specific$ inhibitor, T0070907. The $PPAR{\gamma}$ inhibitor also blocked the ability of ginsenoside Rf to suppress cell migration under hypoxia. The docking simulation results indicate that ginsenoside Rf binds to the active site of $PPAR{\gamma}$. Conclusions: Our results demonstrate that ginsenoside Rf inhibits hypoxia induced-COX-2 expression and cellular migration, which are dependent on $PPAR{\gamma}$ activation. These results suggest that ginsenoside Rf has an antiinflammatory effect under hypoxic conditions. Moreover, docking analysis of ginsenoside Rf into the active site of $PPAR{\gamma}$ suggests that the compound binds to $PPAR{\gamma}$ in a position similar to that of known agonists.

• Journal of Ginseng Research
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• v.42 no.2
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• pp.183-191
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• 2018

Background: Ginseng saponin has long been used as a traditional Asian medicine and is known to be effective in treating various kinds of pain. Ginsenoside Rf is one of the biologically active saponins found in ginseng. We evaluated ginsenoside Rf's antinociceptive and anti-inflammatory effects, and its mechanism of action on adrenergic and serotonergic receptors, in an incisional pain model. Methods: Mechanical hyperalgesia was induced via plantar incision in rats followed by intraperitoneal administration of increasing doses of ginsenoside Rf (vehicle, 0.5 mg/kg, 1 mg/kg, 1.5 mg/kg, and 2 mg/kg). The antinociceptive effect was also compared in a Positive Control Group that received a ketorolac (30 mg/kg) injection, and the $Na{\ddot{i}}ve$ Group, which did not undergo incision. To evaluate the mechanism of action, rats were treated with prazosin (1 mg/kg), yohimbine (2 mg/kg), or ketanserin (1 mg/kg) prior to receiving ginsenoside Rf (1.5 mg/kg). The mechanical withdrawal threshold was measured using von Frey filaments at various time points before and after ginsenoside Rf administration. To evaluate the anti-inflammatory effect, serum interleukin $(IL)-1{\beta}$, IL-6, and tumor necrotizing $factor-{\alpha}$ levels were measured. Results: Ginsenoside Rf increased the mechanical withdrawal threshold significantly, with a curvilinear dose-response curve peaking at 1.5 mg/kg. $IL-1{\beta}$, IL-6, and tumor necrotizing $factor-{\alpha}$ levels significantly decreased after ginsenoside Rf treatment. Ginsenoside Rf's antinociceptive effect was reduced by yohimbine, but potentiated by prazosin and ketanserin. Conclusion: Intraperitoneal ginsenoside Rf has an antinociceptive effect peaking at a dose of 1.5 mg/kg. Anti-inflammatory effects were also detected.

• Archives of Pharmacal Research
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• v.21 no.5
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• pp.615-617
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• 1998

A new dammarane glycoside named ginsenoside $Rf_{2}$ has been isolated from Korean red ginseng (Panax ginseng) and its chemical structure has been elucidated as $6-O-[{\alpha}-L-rham-nopyranosyl (1{\rightarrow}2){\beta}-D-glucopyranosyl]$$dammarane-3{\beta}, 6{\alpa}, 12{\beta}$, 20(R), 25-pentol by chemical and spectral methods.

• Journal of Ginseng Research
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• v.23 no.1 s.53
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• pp.55-59
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• 1999

For the first time we have developed a simple method for conjugation between ginsenoside Rf (Rf) and bovine serum albumin (BSA) or ovalbumin (OVA) by a periodate oxidation method. The Rf-BSA conjugate is confirmed by ultraviolate (UV) scanning, thin layer chromatography (TLC), and SDS-gel electrophoresis. In UV scanning Rf showed three small peaks approximately at 230, 265 and 280 nm. BSA showed a peak at 280 nm. The Rf-BSA conjugate showed right shifted three peaks that BSA alone did not show. In TLC analysis, the Rf-BSA conjugate did not show mobility in silica gel but showed a slight stream of trace. In SDS-gel electrophoresis, Rf-BSA conjugate show a slight less mobility than BSA alone. Rf-OVA conjugate also showed similar patterns with Rf-BSA conjugate. These results demonstrated that periodate oxidation method could be used to produce a stable Rf-BSA or Rf-OV A conjugate and also could be applied for other ginsenoside(s).

• Applied Biological Chemistry
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• v.23 no.4
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• pp.206-210
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• 1980

The minor components of $saponin-ginsenoside-Rf,\;-Rg_2\;and\;-Rh_1$ were isolated from Panax ginseng C.A. Meyer by preparative, semi-preparative and analtical high performance liquid chromatography. The rapid method developed in this work was proved to be very effective in separation and isolation of these minor ginsenosides. A further isolation was achieved by using the recycling technique.

• Journal of Ginseng Research
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• v.45 no.5
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• pp.555-564
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• 2021

Background: Ginsenosides of Panax ginseng are used to enhance skin health and beauty. The present study aimed to investigate the potential use of ginsenoside Rf (Rf) from Panax ginseng as a new anti-pigmentation agent. Methods: The anti-melanogenic effects of Rf were explored. The transcriptional activity of the cyclic adenosine monophosphate (cAMP) response element binding protein (CREB) and the expression levels of tyrosinase, microphthalmia-associated transcription factor (MITF), and tyrosinase-related proteins (Tyrps) were evaluated in melanocytes and UV-irradiated ex vivo human skin. Results: Rf significantly inhibited Forskolin (FSK) or UV-stimulated melanogenesis. Consistently, cellular tyrosinase activity and levels of MITF, tyrosinase, and Tyrps were downregulated. Furthermore, Rf suppressed MITF promoter activity, which was stimulated by FSK or CREB-regulated transcription coactivator 3 (CRTC3) overexpression. Increased CREB phosphorylation and protein kinase A (PKA) activity induced by FSK were also mitigated in the presence of Rf. Conclusion: Rf can be used as a reliable anti-pigmentation agent, which has a scientifically confirmed and reproducible action mechanism, via inhibition of CREB/MITF pathway.

• Korean Journal of Plant Tissue Culture
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• v.27 no.6
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• pp.485-489
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• 2000

The patterns and contents of ginsenosides were examined in normal root parts and hairy root lines of Panax ginseng C. A. Meyer. Ginsenoside-Rb$_1$, -Rb$_2$, -Rc, -Rd, -Re, -Rf, -Rg$_1$, -Rg$_2$ were detected in normal roots and hairy roots of ginseng. The patterns and contents of ginsenosides in that were very difference each other. The contents of total ginsenoside of hairy root (KGHR-1) was 17.42 mg/g dry wt, it's highest compared to others. Ginsenoside contents of hairy root (KGHR-1) was higher on ginsenoside-Rd, Rg$_1$, KGHR-5 was higher on ginsenoside-Rb$_1$, Rg$_1$, and KGHR-8 was higher on ginsenoside-Rd, Re than others. The contents of total ginsenosides on 6 years old ginseng cultured in the field were high in the order of main root, lateral root and fine roots, and content of ginsenosides in fine roots was 3.2 times higher than that in main root. The ratio of ginsenoside-Rg$_1$to total ginsenosides were about 3.43%, 8.68% and 14.18% respectively on fine root, lateral root and main root, it's very lower than that in hairy roots. It is suggested that specific ginsenosides can be produce in cultures of ginseng hairy roots.

• Journal of Ginseng Research
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• v.39 no.2
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• pp.141-147
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• 2015

Background: Adipocytes, which are the main cellular component of adipose tissue, are the building blocks of obesity. The nuclear hormone receptor $PPAR{\gamma}$ is a major regulator of adipocyte differentiation and development. Obesity, which is one of the most dangerous yet silent diseases of all time, is fast becoming a critical area of research focus. Methods: In this study, we initially aimed to investigate whether the ginsenoside Rf, a compound that is only present in Panax ginseng Meyer, interacts with $PPAR{\gamma}$ by molecular docking simulations. After we performed the docking simulation the result has been analyzed with several different software programs, including Discovery Studio, Pymol, Chimera, Ligplus, and Pose View. All of the programs identified the same mechanism of interaction between $PPAR{\gamma}$ and Rf, at the same active site. To determine the drug-like and biological activities of Rf, we calculate its absorption, distribution, metabolism, excretion, and toxic (ADMET) and prediction of activity spectra for substances (PASS) properties. Considering the results obtained from the computational investigations, the focus was on the in vitro experiments. Results: Because the docking simulations predicted the formation of structural bonds between Rf and $PPAR{\gamma}$, we also investigated whether any evidence for these bonds could be observed at the cellular level. These experiments revealed that Rf treatment of 3T3-L1 adipocytes downregulated the expression levels of $PPAR{\gamma}$ and perilipin, and also decreased the amount of lipid accumulated at different doses. Conclusion: The ginsenoside Rf appears to be promising compound that could prove useful in antiobesity treatments.

• KSBB Journal
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• v.5 no.3
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• pp.263-268
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• 1990

New methods have been developed to transform Panax ginseng with Ri plasmids of Agrobacterium rhizogenes 15834 and A. rhizogenes A4. Modified leaf disc method was made feasible to establish hairy root culture even when an axonic plantlet was not available as in the case of P. ginseng. The contents of ginsenosides (Rgl, Rf, Rc, Rbl, and Rb2) in hairy roots. were determined by HPLC. Hairy root cultures, established as liquid culture in MS medium, was produced 0.34~1.19% ginsenosides on dry weight basis, and this result is significantly higher level than that of normal P. ginseng.

• Journal of Pharmacopuncture
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• v.13 no.1
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• pp.63-77
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• 2010

Objectives: The aim of this experiment is to provide an objective differentiation of cultivated ginseng, cultivated wild ginseng, and wild ginseng through component analysis, and to know the change of ginsenoside components in the process for making red ginseng. Methods: Comparative analysis of ginsenoside $Rb_1,\;Rb_2$, Rc, Rd, Re, Rf, $Rg_1,\;Rg_3,\;Rh_1$ and $Rh_2$ from the cultivated ginseng 4 and 6 years, cultivated wild ginseng, and wild ginseng were conducted using High Performance Liquid Chromatography(hereafter HPLC). And the same analyses were conducted in the process of red ginseng. Results: 1. For content comparison of ginsenoside $Rb_1$, Rc, Rd, Rf, $Rg_1$ and $Rh_1$, wild ginseng showed high content, followed cultivated ginseng 4 and 6 years, cultivated wild ginseng showed low content than any other samples. 2. For content comparison of ginsenoside $Rb_2$ and Re, cultivated ginseng 4 years showed high content, followed wild ginseng and cultivated ginseng 6 years, cultivated wild ginseng showed low content than any other samples. 3. For content comparison of ginsenoside $Rg_3$, wild ginseng and cultivated wild ginseng were only showed low content. 4. For content comparison of ginsenoside $Rh_2$, cultivated wild ginseng was only showed low content. 5. In the process of red ginseng, ginsenoside $Rb_1,\;Rb_2$, Rc, Rd, $Rg_3$ and $Rh_1$ were increased, and ginsenoside Re and $Rg_1$ were decreased in cultivated wild ginseng. 6. In the process of red ginseng, ginsenoside $Rg_3$ and $Rh_1$ were increased, and ginsenoside $Rb_2$, Rc, and Re were decreased in cultivated ginseng 4 years. 7. In the process of red ginseng, ginsenoside $Rb_1,\;Rb_2$, Rf and $Rh_1$ were increased, and ginsenoside Rc and Rd were decreased in cultivated ginseng 6 years. Conclusions: Distribution of ginsenoside contents to the cultivated ginseng, cultivated wild ginseng, and wild ginseng was similar and was not showed special characteristics between samples. And the change of ginsenoside to the process of red ginseng, cultivated ginseng and cultivated wild ginseng were showed different aspect.